Names and pronunciation
(al-oh-pure′i-nole) Aloprim, Zyloprim
PDF page 50
Loading InternPractice…
Drug reference
(al-oh-pure′i-nole) Aloprim, Zyloprim
PDF page 50
Func. class.: Antigout drug, antihy- peruricemic
PDF page 50
Chem. class.: Xanthine oxidase inhibitor
PDF page 50
Do not confuse: Zyloprim/Zovirax/zolpidem
PDF page 50
ACTION: Inhibits the enzyme xanthine oxidase, reducing uric acid synthesis
PDF page 50
USES: Chronic gout, hyperuricemia associated with malignancies, recurrent calcium oxalate calculi, uric acid calculi
PDF page 50
CONTRAINDICATIONS: Hyper- sensitivity Precautions: Pregnancy, breastfeeding, children, renal/hepatic disease
PDF page 50
SIDE EFFECTS GI: Nausea, vomiting, malaise, diarrhea, hepatitis INTEG: Rash CV: Hypo- and hypertension, HF (IV use) CNS: Drowsiness GU: Renal failure MISC: Hypersensitivity, bone marrow depression MS: Acute gouty attack
PDF page 51
INTERACTIONS Increase: rash—ampicillin, amoxicillin; avoid concurrent use Increase: action of oral anticoagulants, theophylline Increase: hypersensitivity, toxicity—ACE inhibitors, thiazides Increase: bone marrow depression— (mercaptopurine, azaTHIOprine) Increase: xanthine nephropathy, calculi— rasburicase
PDF page 51
DOSAGE AND ROUTES Increased uric acid levels in malignancies • Adult/child >10 yr: PO 600-800 mg/ day in divided doses for 2-3 days; start up to 1-2 days before chemotherapy; IV INFUSION 200-400 mg/m2/day, 24-48 hr before chemotherapy, may be divided at 6-, 8-, 12-hr intervals; max 600 mg/day • Child 6-10 yr: PO 300 mg/day, adjust dose after 48 hr; max 400 mg/day • Child <6 yr: PO 150 mg/day, adjust dose after 48 hr • Child ≤10 yr: IV INFUSION 200 mg/ m2/day, initially as a single dose or di- vided q6-12hr Recurrent calculi • Adult: PO 200-300 mg/day in a single dose or divided bid-tid Uric acid nephropathy prevention • Adult and child >10 yr: PO 600-800 mg/day × 2-3 days Gout (mild) • Adult: PO 100 mg/day, titrating up- ward, max 800 mg/day Renal dose • Adult: PO/IV CCr 81-100 mL/min 300 mg/day; CCr 61-80 mL/min 250 mg/day; CCr 41-60 mL/min 200 mg/day; CCr 21-40 mL/min 150 mg/day; CCr 10-20 mL/min 100-200 mg/day; CCr 3-9 mL/min 100 mg/day or 100 mg every other day; CCr <3 mL/min 100 mg q24hr or longer or 100 mg every 3rd day
PDF page 50
Available forms: Tablets, scored 100, 300 mg; powder for injection 500 mg/ vial
PDF page 50
Administer: PO route • With meals to prevent GI symptoms; may crush, add to foods or fluids • Begin 1-2 days before antineoplastic therapy Intermittent IV INFUSION route • Use in tumor lysis prior to start of chemotherapy (24-48 hr) • Reconstitute 30-mL vial with 25 mL of sterile water for inj; dilute to desired concentrations (≤6 mg/mL) with 0.9% NaCl for inj or D5W for inj; begin infusion within 10 hr Y-site compatibilities: Acyclovir, ami nophylline, amphotericin B lipid complex, anidulafungin, argatroban, atenolol, aztreonam, bivalirudin, bleomy- cin, bumetanide, buprenorphine, butor- phanol, calcium gluconate, CARBOplatin, caspofungin, ceFAZolin, cefoTEtan, cefTAZidime, ceftizoxime, cefTRIAXone, cefuroxime, CISplatin, cyclophospha- mide, DACTINomycin, DAUNOrubicin citrate liposome, dexamethasone, dex- medetomidine, DOCEtaxel, DOXOrubicin liposomal, enalaprilat, etoposide, famoti- dine, fenoldopam, filgrastim, flucon- azole, fludarabine, fluorouracil, furose- mide, gallium, ganciclovir, gatifloxacin, gemcitabine, gemtuzumab, granisetron hydrochloride, heparin, hydrocortisone phosphate, hydrocortisone succinate, HYDROmorphone, ifosfamide, linezolid injection, LORazepam, mannitol, mesna, methotrexate, metroNIDAZOLE, milri- none, mitoXANtrone, morphine, nesirit- ide, octreotide, oxytocin, PACLitaxel, pamidronate, pantoprazole, PEMEtrexed, piperacillin, piperacillin-tazobactam, plicamycin, potassium chloride, raNITI- dine, sodium acetate, sulfamethoxazole- trimethoprim, teniposide, thiotepa, ticar- cillin, ticarcillin-clavulanate, tigecycline, tirofiban, vancomycin, vasopressin, vin- BLAStine, vinCRIStine, voriconazole, zido vudine, zoledronic acid
PDF pages 50, 51
Assess: • For gout: joint pain, swelling; may use with NSAIDs for acute gouty attacks; effect may take several weeks • CBC, AST, ALT, BUN, creatinine before A starting treatment, periodically • I&O ratio; increase fluids to 2 L/day to prevent stone formation and toxicity • For rash, hypersensitivity reactions, discontinue allopurinol immediately, af- ter rash is resolved, treatment may con- tinue at a lower dose
PDF page 51
Evaluate: • Therapeutic response: decreased pain in joints, decreased stone formation in kidneys, decreased uric acid levels
PDF page 51
CLINICAL CONSIDERATIONS
PDF page 51
Patient and caregiver information: • To take as prescribed; if dose is missed, take as soon as remembered; do not double dose; tablets may be crushed • To increase fluid intake to 2 L/day • To report skin rash, stomatitis, mal- aise, fever, aching; product should be discontinued • To avoid hazardous activities if drows- iness or dizziness occurs • To avoid alcohol, caffeine; will in- crease uric acid levels • An alkaline diet may be required • That follow-up examinations and blood work will be needed • To identify triggers and avoid • To avoid large doses of vitamin C; kidney stone formation may occur • To reduce dairy products, refined sug- ars, sodium, meat if taking for calcium oxalate stones; to identify triggers and avoid
PDF page 51
PHARMACOKINETICS Protein binding <1%, half-life 1-2 hr PO: Peak 1.5 hr; excreted in feces, urine IV: Peak up to 30 min
PDF page 51
• Adult/child >10 yr: PO 600-800 mg/ day in divided doses for 2-3 days; start up to 1-2 days before chemotherapy; IV INFUSION 200-400 mg/m2/day, 24-48 hr before chemotherapy, may be divided at 6-, 8-, 12-hr intervals; max 600 mg/day
PDF page 50
• Child 6-10 yr: PO 300 mg/day, adjust dose after 48 hr; max 400 mg/day
PDF page 50
• Child <6 yr: PO 150 mg/day, adjust dose after 48 hr
PDF page 50
• Child ≤10 yr: IV INFUSION 200 mg/ m2/day, initially as a single dose or di- vided q6-12hr Recurrent calculi
PDF page 50
• Adult: PO 200-300 mg/day in a single dose or divided bid-tid Uric acid nephropathy prevention
PDF page 50
• Adult and child >10 yr: PO 600-800 mg/day × 2-3 days Gout (mild)
PDF page 50
• Adult: PO 100 mg/day, titrating up- ward, max 800 mg/day Renal dose
PDF page 50
• Adult: PO/IV CCr 81-100 mL/min 300 mg/day; CCr 61-80 mL/min 250 mg/day; CCr 41-60 mL/min 200 mg/day; CCr 21-40 mL/min 150 mg/day; CCr 10-20 mL/min 100-200 mg/day; CCr 3-9 mL/min 100 mg/day or 100 mg every other day; CCr <3 mL/min 100 mg q24hr or longer or 100 mg every 3rd day
PDF page 50